反应详情

To a solution of 2-cyclopropyl-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid cyanomethyl-amide (0.19 g, 0.50 mmol) in CH2Cl2 (6 mL) was added trifluoroacetic acid (1.0 mL). The reaction mixture was stirred at room temperature overnight then concentrated. The residue was dissolved in MeOH (10 mL) and H2O (2 mL) and Et3N (2 mL) were added. The reaction mixture was stirred at room temperature overnight then concentrated. The residue was triturated with EtOH to afford 0.093 g (77%) of 2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid carbamoylmethyl-amide as a light yellow solid. MS: (M+H)+=260; mp=215.0-220.0.

1. concentrationthen concentrated
2. dissolutionThe residue was dissolved in MeOH (10 mL)
3. additionH2O (2 mL) and Et3N (2 mL) were added
4. stirringThe reaction mixture was stirred at room temperature overnight
5. concentrationthen concentrated
6. customThe residue was triturated with EtOH